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In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues.
García-Pupo, Laura; Zaldo-Castro, Armando; Exarchou, Vassiliki; Tacoronte-Morales, Juan Enrique; Pieters, Luc; Vanden Berghe, Wim; Nuñez-Figueredo, Yanier; Delgado-Hernández, René.
Afiliação
  • García-Pupo L; Centro de Investigación y Desarrollo de Medicamentos (CIDEM), Ave 26, No. 1605 Boyeros y Puentes Grandes, CP 10600 La Habana, Cuba. laura.garcia@cidem.cu.
  • Zaldo-Castro A; Centro de Estudios de Productos Naturales, Facultad de Química, Universidad de la Habana, Zapata s/n entre G y Carlitos Aguirre, Vedado, Plaza de la Revolución, CP 10400 La Habana, Cuba. zaldo@fq.uh.cu.
  • Exarchou V; Natural Products & Food Research & Analysis (NatuRA), Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, PC 2610 Antwerp, Belgium. vasiliki.exarchou@uantwerpen.be.
  • Tacoronte-Morales JE; Centro de Estudios de Productos Naturales, Facultad de Química, Universidad de la Habana, Zapata s/n entre G y Carlitos Aguirre, Vedado, Plaza de la Revolución, CP 10400 La Habana, Cuba. jetacoronte@yahoo.com.
  • Pieters L; Natural Products & Food Research & Analysis (NatuRA), Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, PC 2610 Antwerp, Belgium. luc.pieters@uantwerpen.be.
  • Vanden Berghe W; Protein Chemistry, Proteomics and Epigenetic Signaling (PPES), Department of Biomedical Sciences, University of Antwerp, Universiteitsplein 1, PC 2610 Antwerp, Belgium. wim.vandenberghe@uantwerpen.be.
  • Nuñez-Figueredo Y; Centro de Investigación y Desarrollo de Medicamentos (CIDEM), Ave 26, No. 1605 Boyeros y Puentes Grandes, CP 10600 La Habana, Cuba. yanier.nunez@cidem.cu.
  • Delgado-Hernández R; Centro de Estudios Investigaciones y Evaluaciones Biológicas (CEIEB), Instituto de Farmacia y Alimentos (IFAL), Universidad de la Habana, Calle 222 #2317/23 y 31 La Coronela, La Lisa, CP 13600 La Habana, Cuba. rdelgado@infomed.sld.cu.
Molecules ; 21(8)2016 Jul 29.
Article em En | MEDLINE | ID: mdl-27483221
Two spirosteroid analogues were synthesized and evaluated for their in vitro neuroprotective activities in PC12 cells, against glutamate-induced excitotoxicity and mitochondrial damage in glucose deprivation conditions, as well as their anti-inflammatory potential in LPS/IFNγ-stimulated microglia primary cultures. We also evaluated the in vitro anti-excitotoxic and anti-inflammatory activities of natural and endogenous steroids. Our results show that the plant-derived steroid solasodine decreased PC12 glutamate-induced excitotoxicity, but not the cell death induced by mitochondrial damage and glucose deprivation. Among the two synthetic spirosteroid analogues, only the (25R)-5α-spirostan-3,6-one (S15) protected PC12 against ischemia-related in vitro models and inhibited NO production, as well as the release of IL-1ß by stimulated primary microglia. These findings provide further insights into the role of specific modifications of the A and B rings of sapogenins for their neuroprotective potential.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Esteroides / Microglia / Fármacos Neuroprotetores / Anti-Inflamatórios Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Cuba País de publicação: Suíça
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Esteroides / Microglia / Fármacos Neuroprotetores / Anti-Inflamatórios Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Cuba País de publicação: Suíça